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脂质体是包封药物纳米载体的理想选择[1],它可以提高被包载物质溶解度,增强物质的稳定性,减少外周不良反应发生,且自身无毒。在肿瘤疾病治疗中,依赖高渗透长滞留(EPR)效应的假设,基于病变区域的组织结构、生理功能和正常组织间的差异,脂质体可使药物输送至肿瘤组织富集,更好地发挥治疗作用[2]。但是,基于EPR效应的纳米制剂在实体瘤内转运的靶向效率仍面临很多质疑[3],所有纳米颗粒(包括脂质体在内)仅有0.7%(中位数)的注射剂量被递送至实体瘤,面临脱颗粒困难、药物释放缓慢等问题[4]。因此在脂质体载体的研究中,针对内源性刺激因素pH[5]、氧化还原反应[6]和酶等[7],外源性刺激因素温度变化[8]、磁场[9]、光等[10],研究者开发出基于刺激响应以及具有主动运输功能的靶向脂质体,以期在目标部位高效、可控地释放运载药物,提高脂质体的靶向性并增强细胞毒性[11]。
Application progress of ROS-responsive liposomes in anti-tumor research
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摘要: 活性氧自由基响应型脂质体是基于肿瘤微环境中活性氧自由基(ROS)高水平表达的特点而制备,可使包载药物在肿瘤部位精准释放。在外加光敏剂后,能进一步增强脂质体中药物的可控性。Abstract: Reactive oxygen species(ROS) responsive liposomes are prepared based on the high level of ROS expression in the tumor microenvironment, enabling precise drug delivery to the tumor site. With the addition of photosensitizer, the controllability of drugs in liposomes can be further enhanced.
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Key words:
- reactive oxygen species /
- liposomes /
- tumor /
- photosensitizer
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